HUP0301592A2 - 16alfa-metil- vagy etil-szubsztituált ösztrogének és ezeket tartalmazó gyógyszerkészítmények - Google Patents

16alfa-metil- vagy etil-szubsztituált ösztrogének és ezeket tartalmazó gyógyszerkészítmények Download PDF

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Publication number: HUP0301592A2
Authority: HU; Hungary
Prior art keywords: compound; treatment; compound according; estrogen; ethyl acetate
Prior art date: 2000-07-28

Application number

HU0301592A

Other languages

English (en)

Hungarian (hu)

Inventor

Hubert Jan Jozef Loozen

Jordi Mestres

Gerrit Herman Veeneman

Original Assignee

Akzo Nobel N.V.

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2000-07-28

Filing date

2001-07-23

Publication date

2003-09-29

2001-07-23 Application filed by Akzo Nobel N.V. filed Critical Akzo Nobel N.V.

2003-09-29 Publication of HUP0301592A2 publication Critical patent/HUP0301592A2/hu

Links

239000000262 estrogen Substances 0.000 title claims abstract description 22
229940011871 estrogen Drugs 0.000 title claims abstract description 21
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title claims abstract description 5
239000008194 pharmaceutical composition Substances 0.000 title claims description 5
238000011282 treatment Methods 0.000 claims abstract description 25
-1 steroid compounds Chemical class 0.000 claims abstract description 11
125000005843 halogen group Chemical group 0.000 claims abstract description 9
125000000217 alkyl group Chemical group 0.000 claims abstract description 8
125000003342 alkenyl group Chemical group 0.000 claims abstract description 7
229920006395 saturated elastomer Polymers 0.000 claims abstract description 7
125000003118 aryl group Chemical group 0.000 claims abstract description 4
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 4
150000001875 compounds Chemical class 0.000 claims description 128
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238000000034 method Methods 0.000 claims description 14
238000002360 preparation method Methods 0.000 claims description 9
239000003814 drug Substances 0.000 claims description 7
239000000546 pharmaceutical excipient Substances 0.000 claims description 5
238000002657 hormone replacement therapy Methods 0.000 claims description 4
230000004913 activation Effects 0.000 claims description 3
229910052801 chlorine Inorganic materials 0.000 claims description 3
239000000460 chlorine Substances 0.000 claims description 3
238000004519 manufacturing process Methods 0.000 claims description 3
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 3
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201000010099 disease Diseases 0.000 claims 1
125000001153 fluoro group Chemical group F* 0.000 claims 1
125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
239000000651 prodrug Substances 0.000 abstract description 13
229940002612 prodrug Drugs 0.000 abstract description 13
125000004432 carbon atom Chemical group C* 0.000 abstract description 8
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract description 3
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 132
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210000004027 cell Anatomy 0.000 description 2
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125000001424 substituent group Chemical group 0.000 description 1
125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
239000000829 suppository Substances 0.000 description 1
238000013268 sustained release Methods 0.000 description 1
239000012730 sustained-release form Substances 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
OSBSFAARYOCBHB-UHFFFAOYSA-N tetrapropylammonium Chemical compound CCC[N+](CCC)(CCC)CCC OSBSFAARYOCBHB-UHFFFAOYSA-N 0.000 description 1
239000005051 trimethylchlorosilane Substances 0.000 description 1
239000006213 vaginal ring Substances 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes

Landscapes

Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Endocrinology (AREA)
Physical Education & Sports Medicine (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Reproductive Health (AREA)
Orthopedic Medicine & Surgery (AREA)
Diabetes (AREA)
Rheumatology (AREA)
Hospice & Palliative Care (AREA)
Psychiatry (AREA)
Gynecology & Obstetrics (AREA)
Steroid Compounds (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

HU0301592A 2000-07-28 2001-07-23 16alfa-metil- vagy etil-szubsztituált ösztrogének és ezeket tartalmazó gyógyszerkészítmények HUP0301592A2 (hu)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP00202697		2000-07-28
PCT/EP2001/008535 WO2002010188A1 (en)	2000-07-28	2001-07-23	16alpha-methyl or ethyl substituted estrogens

Publications (1)

Publication Number	Publication Date
HUP0301592A2 true HUP0301592A2 (hu)	2003-09-29

Family

ID=8171866

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
HU0301592A HUP0301592A2 (hu)	2000-07-28	2001-07-23	16alfa-metil- vagy etil-szubsztituált ösztrogének és ezeket tartalmazó gyógyszerkészítmények

Country Status (25)

Country	Link
US (2)	US7696190B2 (cs)
EP (1)	EP1307471B1 (cs)
JP (1)	JP2004505093A (cs)
KR (1)	KR20030029640A (cs)
CN (1)	CN1220696C (cs)
AR (1)	AR029989A1 (cs)
AT (1)	ATE294812T1 (cs)
AU (2)	AU2001282016B2 (cs)
BR (1)	BR0112791A (cs)
CA (1)	CA2416311C (cs)
CZ (1)	CZ2003270A3 (cs)
DE (1)	DE60110606T2 (cs)
EC (1)	ECSP034448A (cs)
ES (1)	ES2241854T3 (cs)
HR (1)	HRP20030060A2 (cs)
HU (1)	HUP0301592A2 (cs)
IL (2)	IL153934A0 (cs)
IS (1)	IS6692A (cs)
MX (1)	MXPA03000845A (cs)
NO (1)	NO20030419L (cs)
PE (1)	PE20020331A1 (cs)
PL (1)	PL366235A1 (cs)
SK (1)	SK882003A3 (cs)
WO (1)	WO2002010188A1 (cs)
ZA (1)	ZA200300417B (cs)

Families Citing this family (5)

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EP1470151B1 (en) *	2002-01-21	2009-12-30	N.V. Organon	Process for the preparation of 7-alpha-methylsteroids
DE10213371C1 (de) *	2002-03-21	2003-12-24	Schering Ag	Verfahren zur Herstellung von 7alpha-Methylsteroiden
CN101014610B (zh) *	2004-09-08	2012-08-22	Msd欧斯股份有限公司	具有选择性雌激素活性的15β-取代的类固醇
UA89964C2 (ru) *	2004-09-08	2010-03-25	Н.В. Органон	15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
CN114409717B (zh) *	2021-12-17	2023-03-17	湖南科益新生物医药有限公司	替勃龙中间体醚化物和替勃龙的制备方法

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DE1084261B (de) *	1957-04-11	1960-06-30	Syntex Sa	Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate
NL226738A (cs) *	1957-04-11
US3257429A (en) *	1957-11-12	1966-06-21	Syntex Corp	16-methylene derivatives of estrone and estradiol
US3007946A (en) *	1958-11-06	1961-11-07	Searle & Co	3-alkoxy-16-methylene-1, 3, 5(10)-estratrien-17-ones
US3049555A (en) *	1959-12-22	1962-08-14	Searle & Co	3-alkoxy-16-methyl-1, 3, 5 (10)-estratrien-17-ones
US3092645A (en) *	1961-12-28	1963-06-04	Searle & Co	Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols
GB1110792A (en) *	1964-04-07	1968-04-24	Res Inst Medicine Chem	Novel 5(10)-dehydro-steroids
US3299108A (en) *	1965-10-18	1967-01-17	Searle & Co	17alpha-alkynyl/alkenyl-13beta-alkyl-11-alkylgona-1, 3, 5 (10)-triene-3, 17beta-diols, ethers and esters thereof and intermediates thereto
US3465010A (en) *	1966-11-22	1969-09-02	Searle & Co	17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof
US3377366A (en) *	1966-12-02	1968-04-09	Searle & Co	17alpha-alkynyl/alkenyl-11, 13beta-dialkylgon-5(10)-en-3-ones and esters thereof
ZA712312B (en)	1970-04-28	1972-01-26	Ochsner Med Found Alton	4,14-estradiene compounds
US3652606A (en) *	1970-08-07	1972-03-28	Searle & Co	3-oxygenated 11beta-methylestr-4-en-17beta-ol and esters thereof
US3704253A (en) *	1970-09-23	1972-11-28	American Home Prod	13 - polycarbonalkyl - 16 - methylgona-1,3,5(10)-trienes and 13-polycarbonalkyl-16-methylgon - 4 - en-3-ones and intermediates for their production
FR2377419A1 (fr) *	1977-01-13	1978-08-11	Roussel Uclaf	Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament
DE2757157C3 (de)	1977-12-19	1980-10-09	Schering Ag, 1000 Berlin Und 4619 Bergkamen	Verfahren zur Herstellung von 16 a -alkylierten Steroiden
AU572589B2 (en)	1983-12-14	1988-05-12	Upjohn Company, The	11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids
US5116830A (en) *	1984-08-17	1992-05-26	Sri International	Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses
DE3822770A1 (de) *	1988-07-01	1990-01-04	Schering Ag	13-alkyl-11ss-phenylgonane
ZA94715B (en)	1993-02-08	1994-10-24	Akzo Nv	Steroids for treating menopausal complaints
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CA2319765A1 (en)	1998-03-09	1999-09-16	Akzo Nobel Nv	New contraceptive kit
TR200003743T2 (tr) *	1998-06-19	2001-07-23	Akzo Nobel N.V.	Testosteron türevi.
WO2000031112A1 (en)	1998-11-20	2000-06-02	Akzo Nobel N.V.	Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11
TW548277B (en) *	1999-07-16	2003-08-21	Akzo Nobel Nv	Orally active androgens
NZ517281A (en) *	1999-09-06	2003-09-26	Akzo Nobel Nv	Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11

2001
- 2001-07-23 US US10/343,293 patent/US7696190B2/en not_active Expired - Fee Related
- 2001-07-23 SK SK88-2003A patent/SK882003A3/sk unknown
- 2001-07-23 IL IL15393401A patent/IL153934A0/xx active IP Right Grant
- 2001-07-23 EP EP01960546A patent/EP1307471B1/en not_active Expired - Lifetime
- 2001-07-23 CN CNB018133983A patent/CN1220696C/zh not_active Expired - Fee Related
- 2001-07-23 CZ CZ2003270A patent/CZ2003270A3/cs unknown
- 2001-07-23 MX MXPA03000845A patent/MXPA03000845A/es active IP Right Grant
- 2001-07-23 DE DE60110606T patent/DE60110606T2/de not_active Expired - Lifetime
- 2001-07-23 AU AU2001282016A patent/AU2001282016B2/en not_active Ceased
- 2001-07-23 HU HU0301592A patent/HUP0301592A2/hu unknown
- 2001-07-23 AU AU8201601A patent/AU8201601A/xx active Pending
- 2001-07-23 JP JP2002515917A patent/JP2004505093A/ja not_active Withdrawn
- 2001-07-23 AT AT01960546T patent/ATE294812T1/de not_active IP Right Cessation
- 2001-07-23 PL PL01366235A patent/PL366235A1/xx unknown
- 2001-07-23 HR HR20030060A patent/HRP20030060A2/hr not_active Application Discontinuation
- 2001-07-23 CA CA002416311A patent/CA2416311C/en not_active Expired - Fee Related
- 2001-07-23 WO PCT/EP2001/008535 patent/WO2002010188A1/en not_active Ceased
- 2001-07-23 KR KR10-2003-7001186A patent/KR20030029640A/ko not_active Withdrawn
- 2001-07-23 ES ES01960546T patent/ES2241854T3/es not_active Expired - Lifetime
- 2001-07-23 BR BR0112791-8A patent/BR0112791A/pt not_active IP Right Cessation
- 2001-07-25 PE PE2001000751A patent/PE20020331A1/es not_active Application Discontinuation
- 2001-07-26 AR ARP010103558A patent/AR029989A1/es unknown
2003
- 2003-01-14 IL IL153934A patent/IL153934A/en not_active IP Right Cessation
- 2003-01-15 ZA ZA200300417A patent/ZA200300417B/xx unknown
- 2003-01-20 IS IS6692A patent/IS6692A/is unknown
- 2003-01-24 EC EC2003004448A patent/ECSP034448A/es unknown
- 2003-01-27 NO NO20030419A patent/NO20030419L/no not_active Application Discontinuation
2009
- 2009-05-29 US US12/475,096 patent/US20100029603A1/en not_active Abandoned

Also Published As

Publication number	Publication date
ES2241854T3 (es)	2005-11-01
IL153934A0 (en)	2003-07-31
WO2002010188A1 (en)	2002-02-07
EP1307471A1 (en)	2003-05-07
ATE294812T1 (de)	2005-05-15
PE20020331A1 (es)	2002-04-30
EP1307471B1 (en)	2005-05-04
SK882003A3 (en)	2003-07-01
AR029989A1 (es)	2003-07-23
US20040043976A1 (en)	2004-03-04
PL366235A1 (en)	2005-01-24
AU2001282016B2 (en)	2005-11-10
US20100029603A1 (en)	2010-02-04
NO20030419D0 (no)	2003-01-27
HRP20030060A2 (en)	2004-06-30
CN1220696C (zh)	2005-09-28
BR0112791A (pt)	2003-06-24
ECSP034448A (es)	2003-03-10
DE60110606D1 (de)	2005-06-09
CN1444596A (zh)	2003-09-24
MXPA03000845A (es)	2004-04-05
KR20030029640A (ko)	2003-04-14
AU8201601A (en)	2002-02-13
IS6692A (is)	2003-01-20
DE60110606T2 (de)	2005-12-01
CZ2003270A3 (cs)	2003-06-18
CA2416311C (en)	2009-04-28
CA2416311A1 (en)	2002-02-07
IL153934A (en)	2007-07-24
JP2004505093A (ja)	2004-02-19
US7696190B2 (en)	2010-04-13
NO20030419L (no)	2003-01-27
ZA200300417B (en)	2004-04-15

Publication	Publication Date	Title
HUT60280A (en)	1992-08-28	Process for producing androgen derivatives inhibiting sexual steroidal activity, as well as pharmaceutical compositions comprising same
US20100120736A1 (en)	2010-05-13	Mineralocorticoid Receptor Antagonists
JP2000256390A (ja)	2000-09-19	性ステロイド活性を抑制するために用いるエストロゲン核誘導体の医薬組成物
JP2001524487A (ja)	2001-12-04	アンドロゲンステロイド化合物並びにその調製法及び使用法
US20100029603A1 (en)	2010-02-04	16alpha-methyl or ethyl substituted estrogens
KR19980071540A (ko)	1998-10-26	피임 및 항-골다공증 활성을 갖는 스테로이드 화합물
AU770331B2 (en)	2004-02-19	Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11
EP0338065B1 (fr)	1994-01-26	Derives de la 19-nor progesterone, leur preparation et leur utilisation
AU2001282016A1 (en)	2002-05-09	16alpha-methyl or ethyl substituted estrogens
EP0437552A1 (fr)	1991-07-24	Derives alcoyles en 17/21 de la 19-nor progesterone
FR2625505A2 (fr)	1989-07-07	Nouveaux derives steroides substitues en 11beta leur procede de preparation et leur application comme medicaments et les compositions pharmaceutiques les renfermant
CN101014610B (zh)	2012-08-22	具有选择性雌激素活性的15β-取代的类固醇
US6949531B2 (en)	2005-09-27	14 β, 16, 17-methylene steroids as novel androgens
CN1481388A (zh)	2004-03-10	具有雄激素-孕激素混合活性的14(15)-不饱和的15-和/或16-取代的雄激素类
GB2185257A (en)	1987-07-15	10 beta (-Alkynyl-4,9(11)-estradiene derivatives and process for their preparation
JP2008546669A (ja)	2008-12-25	アンドロゲンおよびプロゲスタゲンの混合特性を有するステロイド
KR20040039346A (ko)	2004-05-10	호르몬 효과를 갖는 17알파-히드록시-14베타-스테로이드
KR20070061557A (ko)	2007-06-13	선택적 에스트로겐 활성을 보이는 15β-치환 스테로이드
HK1052012B (en)	2005-06-10	16, 17-carbocyclic condensed steroid compounds having selective estrogenic activity